• Tobacco use is the leading preventable cause of premature death in Canada
  • Nicotine addiction is regarded as a chronic medical condition; now classified in the Diagnostic and Statistical Manual of Mental Disorders as tobacco use disorder
  • Prevalence in Canada is approximately 16 %; in Saskatchewan over 20 %

Detrimental effects of tobacco use include:

  • Cardiovascular disease – coronary heart disease, stroke, peripheral vascular disease, etc.
  • Respiratory disease – COPD, exacerbation of asthma, lung cancer
  • Other cancers – bladder, cervix, colorectal, oral and esophageal, kidney, liver, pancreas, stomach
  • Decreased fertility, erectile dysfunction, pregnancy-related disorders
  • Cataracts, age-related macular degeneration
  • Tooth stains, Gum disease
  • Type 2 diabetes mellitus
  • Osteoporosis
  • Rheumatoid arthritis

Benefits of quitting:

  • After 1 year, reduced risk of heart attack
  • Within 2 – 5 years, risk of stroke returns to baseline
  • Within 5 years, risk of oral, esophageal and bladder cancers decrease by 50 %
  • After 10 years, risk of lung cancer decreases by 50 %
  • Improved overall health, fewer sick days
  • Offer efficacious pharmacotherapy to every patient who smokes 10 or more cigarettes daily and is willing to make a quit attempt (Level 1A Recommendation)
    •  Utilize PACT/TAR program for routine screening of patients who smoke or use tobacco and for the identification of those where initiating pharmacotherapy is indicated

  • All patients who smoke/use tobacco should be offered assistance and/or pharmacotherapy; however, evidence suggests we focus on those who smoke more than 10 cigarettes daily
  • Age under 18 years old

  • Pregnant or breastfeeding

  • Unstable cardiovascular disease
    • Myocardial infarction within 14 days
    • Persistent unexplained chest pain

  • Unstable psychiatric illness

  • History of suicidal ideation/attempt(s)

  • History of anorexia or bulimia

  • End-stage renal disease

  • Signs/symptoms of undiagnosed or inadequately controlled smoking-related diseases e,g, COPD, lung cancer
  • Combining counseling and smoking cessation medication is more effective than either alone, therefore both should be provided to patients/clients trying to stop smoking where feasible. (Level 1A Recommendation)
    • For the purposes of the minor ailment program, you may prescribe a pharmacologic agent WITHOUT having the patient go through the PACT or TAR program. These are still strongly suggested, but if the patient is not interested, you may still prescribe treatment.
  • While varenicline has the highest quit rates, therapy should be tailored to the individual’s needs and preferences. (Level 1C Recommendation)
  • Combination pharmacotherapy may be warranted in cases of previous unsuccessful attempts with monotherapy, or patient preference.
1. Non-pharmacological treatments for tobacco cessation:
  • Counseling and psychosocial support programs (e.g. PACT program).
    • Cognitive Behavioral Therapy
    • Motivational Interviewing
      • Explore the “5 Rs” using reflective listening:
        • Relevance
        • Rewards
        • Risk
        • Roadblocks
        • Repetition
    • Spiritual / Religious / Cultural Support (e.g. TAR program)
  • “Cold Turkey” Approach (sudden discontinuation of smoking and/or tobacco-use)
    • Offer supportive counseling and arrange follow-up
2. OTC drug options:
  • Nicotine replacement therapy (NRT)
    • Nicotine patch
      • Improves smoking cessation rates at 6 and 12 months compared to placebo (Level 1A Evidence)
    • Nicotine gum
      • May improve smoking cessation rates at 6 and 12 months compared to placebo (Level 1B Evidence)
    • Nicotine oral inhaler
      • May improve smoking cessation rates at 6 and 12 months compared to placebo (Level 2C Evidence)
    • Nicotine lozenge
      • May improve smoking cessation rates at 6 and 12 months compared to placebo (Level 2C Evidence)
    • Nicotine oral mist
      • May provide rapid relief of cravings; insufficient evidence to provide evidence rating for cessation
    • Nicotine nasal spray {Available in the USA}
      • Improves smoking cessation rates at 6 and 12 months compared to placebo (Level 2C Evidence)
    • Nicotine sublingual tablet {Available in the USA}
      • May improve smoking cessation rates at 6 and 12 months compared to placebo (Level 2C Evidence)
    • Reduce to Quit Approach (+ nicotine gum)
      • Step 1: (0-6 weeks) Smoker sets a target for no. of cigarettes per day to cut down (at least 50% recommended) and a date to achieve it by. Smoker uses gum to manage cravings.
      • Step 2: (6 weeks up to 6 months) Smoker continues to cut down cigarettes using gum. Goal should be complete stop by 6 months. Smoker should seek advice from healthcare professional if smoking has not stopped within 9 months.
      • Step 3: (within 9 months) Smoker stops all cigarettes and continues to use gum to relieve cravings.
      • Step 4: (within 12 months) Smoker cuts down the amount of gum used, then stops gum use completely (within 3 months of stopping smoking).
    • Contraindications: avoid for 2 weeks after myocardial infarction, in patients with serious arrhythmias or severe or worsening angina.
    • Cautions: hyperthyroidism (tachycardia, angina), pheochyromocytoma (hypertensive crisis), insulin-dependent diabetes (increased risk of hypoglycemia). Of particular concern if patient continues to smoke while using NRT.
    • Cytisine (Cravv)
      • Natural product derived from Golden Rain or Golden Chain acacia
      • Mechanism of action: partial nicotine agonist
      • Evidence suggests efficacy similar or better than NRT
      • Complex dosing regimen requiring multiple daily doses
      • Adverse effects: nausea, vomiting, sleep disorders
3. Prescription drug options:
  • Health Canada and product monographs recommend that NRT therapy be considered first before prescribing bupropion or varenicline, but a trial of NRT may be skipped if patient prefers alternate treatment.
  • Varenicline (Champix®, generic)
    • Varenicline improves smoking cessation rates at 6 and 12 months compared to placebo (Level 1A Evidence). Also higher cessation rates compared to Bupropion and NRT (Level 1A Evidence).
    • Dosage:
      • Days 1-3: 0.5mg orally once daily
      • Days 4-7: 0.5mg orally twice daily
      • Days 8 to End of treatment: 0.5mg orally twice daily; OR, 1mg orally twice daily
        • Maintenance dose selected depends on patient response and tolerability
        • Less nausea reported with 0.5mg BID option
        • Similar success rates seen with both dosing strategies, compared to placebo
      • Start varenicline 1-2 weeks before planned ‘quit date'
        • Some literature suggests no difference in cessation success with setting quit date between days 8 and 35 of varenicline therapy.
    • Total treatment duration recommended is 12 weeks. For patients who have successfully stopped smoking at the end of 12 weeks, an additional course of 12 weeks treatment with varenicline may be considered; however, the Saskatchewan Prescription Drug Plan (SPDP) will only cover 12 weeks of therapy per 365-day period.
    • After completing a course of treatment, tapering is not required.
    • CAUTION in patients with:
      • Severe renal impairment (CrCl <30ml/min): maximum of 0.5mg BID dosing
      • History of suicidal ideations or current unstable psychiatric illness
      • Unstable cardiovascular disease
    • No significant drug interactions
  • Bupropion (Zyban®)
    • Bupropion improves smoking cessation rates at 6 months (Level 1A Evidence) and may improve smoking cessation rates at 12 months (Level 1B Evidence) compared to placebo. Similar cessation rates to NRT (Level 1B Evidence).
    • Dosage:
      • Days 1-3: 150mg SR orally once daily
      • Day 4 to End of treatment: 150mg SR orally twice daily
    • Quit smoking 1-2 weeks after starting Zyban®
    • 12 week course; longer courses do not improve cessation rates
    • AVOID in patients with a history of seizure disorder or eating disorder
    • CAUTION in patients with:
      • Renal (CrCl <90ml/min) or hepatic dysfunction
      • Seizure risk factors
        • Medications which lower seizure threshold
        • CNS tumour
        • Diabetes treated with insulin
      • Unstable psychiatric illness
    • Bupropion has many drug interactions (strongly inhibits 2D6):
      • 2D6 drugs: SSRIs, TCAs, beta blockers, antipsychotics, antiarrythmics
      • Drugs that lower seizure threshold: antidepressants, antipsychotics, theophylline, antimalarials, sedating antihistamines
      • MAO inhibitors within 14 days: hypertensive crisis likely
    • Must use Zyban® brand for the assessment fee to be covered by DPEBB
  • Combination treatment
    • Varenicline +nicotine patch vs. varenicline alone: Higher rates of abstinence at 36 weeks vs. varenicline (Level of Evidence 1B)
    • Varenicline + bupropion vs varenicline alone: No better at 52 weeks (Level of Evidence 1B)
    • Bupropion + NRT vs. NRT alone: No difference
  • Second line pharmacotherapy - not officially indicated for smoking cessation. This information is provided for completeness. These agents are not currently in the scope of pharmacist prescribing but could be recommended as options if contraindications, intolerance to first line agents.
    • Nortriptyline improves smoking cessation rates at 6 months (Level 2A Evidence) compared to placebo.
      • Dosage: Total treatment duration of 12 weeks
        • Start at 25mg per day, bedtime dosing preferred, beginning 10-28 days prior to quit date
        • Increase gradually to 75 - 100 mg / day once daily or up to QID
      • AVOID in patients with history of seizure disorder or cardiovascular disease
      • CAUTION in elderly due to major sedation potential and other anticholinergic side effects.
      • CAUTION if patient is on other serotonergic drugs due to additive risk of serotonin syndrome.
    • Clonidine may be effective for smoking cessation; lower level of evidence
      • Dosage: Duration of therapy 3 to 10 weeks, must be tapered when discontinuing
        • Start with 0.1 mg BID on or up to 3 days prior to quit date
        • Increase by 0.1 mg/day once weekly up to 0.4 mg daily as needed
      • Caution in combination with antihypertensive agents due to additive hypotensive effect
      • Adverse effects are common - sedation, dizziness, dry mouth

Assess Benefit:

  • Follow-up with patient to assess tolerability, benefit, and inquire about any abnormal changes in mood in 2-4 weeks or as per patient preference
    • The PACT/TAR program structure and resources are a useful guides for performing follow-up and continued counseling
  • If cessation unsuccessful after 12 weeks, assess adherence, technique (i.e.: for NRT), and possible factors contributing to poor efficacy (i.e.: choosing a quit date too late in therapy, major life events, peer pressure, etc.) that may be avoidable or manageable in a subsequent quit attempt. Then:
    1. Consider different first line therapy:
      • NRT, buproprion SR, varenicline
    2. Combination therapy of varenicline + NRT may be attempted, though consider increased cost and increased side effects
  • If cessation successful after 12 weeks, an additional 12 weeks of therapy may be considered, or a taper if using varenicilne.

Assess Adverse Effects:

  • IMPORTANT: Smoking cessation with or without treatment is associated with various symptoms. For example, dysphoric or depressed mood, insomnia, irritability, frustration or anger, anxiety, difficulty concentrating, restlessness, decreased heart rate, increased appetite or weight gain have been reported in patients attempting to stop smoking.
  • Post-marketing reports of serious neuropsychiatric symptoms in patients being treated with varenicline (Champix®), including depressed mood, agitation, aggression, hostility, changes in behavior, suicide related events, including ideation, behavior, attempted suicide and suicide, as well as worsening of pre-existing psychiatric disorder.
    • These events have occurred in patients with and without pre-existing psychiatric disorders
    • Refer any patient experiencing the above neuropsychiatric symptoms to his/her physician or, in the case of suicidal ideation, to his/her local emergency department
  • Weight gain
    • Smoking cessation is associated with an average increase of 4-5kg ("9-11lbs) in body weight after 12 months of abstinence, with most weight gain occurring within 3 months of quitting
    • Variation in weight gain is large, with about 16% of quitters losing weight and 13% gaining more than 10kg
    • More cigarettes smoked is associated with more weight gained
    • Bupropion and NRT (4mg gum/lozenge) both delay weight gain
    • Encourage patients to follow healthy lifestyle measures (i.e.: healthy diet and exercise) to minimize weight gain
  • Nausea
    • Varenicline:
      • Initial nausea: Try taking after eating with a full glass of water
      • Ongoing nausea: Consider switching to 0.5mg orally twice daily maintenance dosing strategy (versus 1mg orally twice daily)
  • Insomnia
    • Varenicline: Consider taking second dose earlier in the day (i.e.: with supper or late afternoon snack)
    • Bupropion: Take second dose of the day "8 hours prior to bedtime, but >6 hours after first dose (to reduce seizure potential)
  • Dry Mouth
    • Bupropion: Chew on ice chips or sugarless gum

Other Support:

  • Offer PACT/TAR resources such as “What Happens When You Smoke”, “Benefits of Quitting", “Top 10 Reasons To Quit”, “Smoking Reduction Tips”, and other resources available from PACT/TAR website (makeapact.ca)
  • Offer a referral to the Smokers’ Helpline

Effect of Quitting Smoking on Medications:

  • Physiological changes resulting from smoking cessation, with or without pharmacotherapy treatment, may alter the pharmacokinetics or pharmacodynamics of some drugs for which dosage adjustment may be necessary (examples include clozapine, theophylline, warfarin and insulin). As smoking induces cytochrome P450 (CYP) isoenzyme 1A2, smoking-cessation may result in an increase of plasma levels of CYP1A2 substrates and therefore medications metabolized by CYP1A2 will no longer exhibit the same extensive metabolism, leading to an increase in serum levels of such medications.

Drug

Effect of Smoking

Management after smoking cessation

Caffeine

'1' metabolism

4, caffeine intake by half;
Monitor for caffeine toxicity

Clozapine

'1' metabolism

(4, plasma

concentrations by 18%)

Monitor for clozapine toxicity; dose 4, may be needed

Flecainide

'1' metabolism (~17% higher dose requirement)

Dose 4, may be needed

Fluvoxamine

'1' metabolism
(4, AUC by 30%)

Dose 4, not usually needed;
monitor for side-effects

Insulin

'1' insulin
requirements

Monitor for episodes of hypoglycemia

Mexiletine

'1' metabolism

Dose 4' may be needed; monitor for adverse effects

Olanzapine

'1' metabolism (minimal decrease in plasma concentration)

Dose 4' may be needed;
monitor for adverse effects

Propranolol

'1' metabolism

Dose 4' may be needed;
monitor for adverse effects

Theophylline

'1' metabolism

Monitor levels and 4' dose accordingly; decrease often needed

Warfarin

INR increases
reported

Monitor INR 3-5 days after cessation and adjust dose if needed

 

Detailed information on contraindications, cautions, adverse effects and interactions is available in individual drug monographs in RxTx - CPS from CPhA, RxTx (internet), Lexi-Comp, AHFS, www.drugs.com or other reliable drug monograph references. For comprehensive drug comparisons, see RxFiles charts (www.rxfiles.ca). This information should be routinely consulted before prescribing.

OTC Products

 

Formulation

Dosage

Instructions

Duration

Nicotine Patch

More than 20 cigarettes per day: 1 patch (21mg/24 h) daily x 3-4 weeks (21mg: 6 weeks, 14 mg: 2-4 weeks, 7 mg: 2-4 weeks)

Less than 20 cigarettes per day: 1 patch (14mg/24 h) daily x 3-4 weeks

Tapering: reduce strength of patch (e.g. from 21 to 14 to 7 mg/24h) every 3-4 weeks.

* Heavy smokers may require more than one patch initially

* For patients who weigh less than 100 lbs (45 kg) start with 14 mg patch

- Apply patch to a dry, hairless area between neck and waist - Nicotine patches should be changed daily (i.e. old patch should be removed before a new patch is applied)

- Application sites should be rotated to avoid skin irritation

- Patch may be removed at bedtime if patient complains of insomnia and/or vivid dreams

- Apply pressure to the patch for 10 seconds when applying to avoid detachment

8 - 12 weeks

 * It may be

Necessary for some to remain on NRT longer than suggested in monograph

 

Nicotine
Gum

1 to 24 cigs/day - 2 mg gum (up to 20 pcs/day)

25+ cigs/day - 4 mg gum (up to 20 pcs/day)

Recommended chewing on a fixed schedule for the first month of therapy. Pack-a-day smoker could chew one piece of gum per hour.

Tapering: reduce by one piece per day each week as withdrawal symptoms allow

Can also be used PRN

2 mg gum provides 1 mg of nicotine 4 mg gum provides 1.5 to 2 mg of nicotine

Bite the gum to release nicotine - feel tingle

- Park between cheek and the gums

- Once tingle subsides (about 1 minute), chew again until tingle returns

- Park again and repeat the process

- After 30 minutes the tingle does not return

- Discard gum

- May want to chew gum 30 minutes before coffee if coffee is a trigger

- Avoid acidic beverages while chewing

1-3 months PRN use may be necessary after 3 months

 

Nicotine
Inhaler

One Cylinder = 20 minutes of puffing (or 400 puffs of nicotine vapor absorbed through lining of mouth and throat)

- Puff 5-10 minutes at a time, just as a cigarette

- Use 6 to 12 times a day for 3 to 12 weeks

- Gradually reduce over another 6 to 12 weeks if needed

80 puffs equals one cigarette

- Avoid acidic beverages while using the inhaler

- Wash mouthpiece daily with soap and water

12 - 24 Weeks

Nicotine
Lozenge

Thrive Nicotine Lozenge:

- Less than 20 cigs/day use 1 mg lozenge (5 to 10 lozenges/day for first 2 weeks, 3 to 8 lozenges/day for next 2 weeks, 3 to 5 lozenges/day for month 2, 2 to 3 lozenges/day for month 3, and as needed for months 4 to 6)

- More than 20 cigs/day use 2 mg lozenge (15 lozenges/day for first 2 weeks, 12 lozenges/day for next 2 weeks, 10 lozenges/day for month 2, 5 lozenges/day for month 3, as needed for months 4 to 6)

Nicorette Lozenge:

- smoke first cigarette within 30 minutes of waking: use 4 mg lozenge (about 15 pieces/day for 3 months, then gradually reduce number of lozenges or switch to 2 mg dose)

- smoke first cigarette more than 30 minutes after waking: use 2 mg lozenge (about 15 pieces/day for 3 months, then gradually reduce number of lozenges

Suck on lozenge until taste is strong

- Place lozenge between cheek and gum until taste is gone

- Repeat until dissolved (about 30 minutes)

- useful for people with dentures and jaw problems

- Avoid food and drink for 15 minutes before using and acidic beverages for 30 minutes

 

12 weeks

 

Nicotine
Spray

- Highly individualized dosing. Provides 1mg of nicotine per spray. Use enough to control cravings

- Use a spray when would normally smoke a cigarette or having cravings to smoke.

- Use a second spray if cravings do not disappear within a few minutes

- On average, 1-2 sprays every 30 minutes to an hour is required initially

- Maximum of 2 sprays per dose, or 4 sprays per hour. Maximum of 64 sprays per day.

- Spray on or under the tongue. Do not spray directly into the throat and do not inhale when spraying.

- Avoid eating and drinking 15 minutes before or after use of the spray.

 

1-3 months, but may be necessary to use PRN after 3 months.

 

 

Prescription Products

Drug

Dosage

Duration

Comments

Varenicline
(Champix®)

Quit 1-2 weeks after starting varenicline.

Days 1-3: 0.5mg orally once daily

 Days 4-7: 0.5mg orally twice daily

 Days 8 to End of treatment:

0.5mg orally twice daily; OR, 1mg orally twice daily

12 weeks

 

Additional 12 weeks may be considered if high potential for relapse

 

Maintenance dose selected depends on patient response and tolerability

- Less nausea reported with 0.5mg BID option

- Similar success rates seen with both dosing strategies, compared to placebo, but more evidence for 1mg BID

Bupropion SR
(Zyban®)

Quit 1-2 weeks after starting bupropion

Days 1-3: 150mg SR orally once daily

Day 4 to End of treatment:

150mg SR orally twice daily

12 weeks

 

Must use Zyban® brand for the assessment fee to be covered by DPEBB

 - Additional 12 weeks of therapy NOT beneficial for preventing relapse

 

Nortriptyline

Quit 10-28 days after starting nortriptyline

 

Begin at 75mg per day at bedtime

12 weeks

 

- Pharmacists cannot prescribe

Off-label use. Only consider if other first-line therapies were intolerable.

May start with a lower dose if sedation a major side effect

Caution in elderly

Many drug interactions

 

 

  • Fee pseudoDIN 00951321; maximum of two claims per 365 days

  • May claim both the minor ailment prescribing fee and relevant PACT fees (if trained)

  • May prescribe enough for 12 weeks of therapy. For varenicline, may provide 1 refill for patients who need longer therapy

  • If choosing Bupropion SR as treatment, must use Zyban® brand for the assessment fee to be covered by DPEBB

  • Only products with an official indication from Health Canada for tobacco cessation and/or recommended by reputable and reliable guidelines are considered for these guidelines.
  1. CAN-ADAPTT. (2012). Canadian Smoking Cessation Clinical Practice Guideline. Toronto, Canada: Canadian Action Network for the Advancement, Dissemination and Adoption of Practice-informed Tobacco Treatment, Centre for Addiction and Mental Health.
  2. NHS Clinical Knowledge Summaries. Smoking Cessation. Available at http://cks.nice.org.uk/smoking-cessation#!management. Accessed August 2013.
  3. Cressman A, et al. Smoking Cessation Therapy During Pregnancy. Canadian Family Physician. 2012. 58:5525-527. 
  4. Bupropion SR (Zyban®) Product Monograph. In RxTx online database. Available from www.e-therapeutics.ca. (By subscription). Available in Saskatchewan through SHIRP (www.shirp.ca).
  5. Varenicline (Champix®) Product Monograph. In RxTx online database. Available from www.e-therapeutics.ca. (By subscription). Available in Saskatchewan through SHIRP (www.shirp.ca).
  6. Gray K, et al. Varenicline versus Bupropion XL for Smoking Cessation in Older Adolescents: A Randomized, Double-Blind Pilot Trial. Nicotine & Tobacco Research. 2012. 14(2):234-239.
  7. Partnership to Assist with Cessation of Tobacco (PACT) and Tobacco Addiction Recover (TAR). (2012). Pharmacists’ Association of Saskatchewan.
  8. Rennard S, et al. A Randomized Placebo-Controlled Trial of Varenicline for Smoking Cessation Allowing Flexible Quit Dates. Nicotine & Tobacco Research. 2012. 14(3):343-350.
  9. RxFiles. Tobacco / Smoking Cessation Pharmacotherapy. 2012. Available at www.rxfiles.ca
  10. UpToDate. Pharmacotherapy for Smoking Cessation in Adults. 2012.
  11. Zwar N, et al. Nicotine and nicotine replacement therapy – the facts. Australian Pharmacist. 2006;25(12):969-973.
  12. Fagerstrom K, et al. Stopping smokeless tobacco with varenicline: randomised double blind placebo controlled trial. BMJ. 2010;341:c6549.
  13. Aubin H, et al. Weight gain in smokers after quitting cigarettes: meta-analysis. BMJ. 2012;345:e4439.
  14. Health Canada. CHAMPIX (varenicline tartrate) and ZYBAN (bupropion hydrochloride) - Revision to the Consumer Information of Non-Nicotine Smoking Cessation Aids - For the Public. Available at http://www.healthycanadians.gc.ca/recall-alert-rappel-avis/hc-sc/2013/33623a-eng.php. Accessed August, 2013.

No part of this work may be reproduced, distributed, or transmitted in any form or by any means, including photocopying, recording, or other electronic or mechanical methods, without the prior written permission of the copyright holder. For copyright permission requests, please contact druginfo@usask.ca.

Prepared by: Jaris Swidrovich, BSP, PharmD Student
Reviewed by: Carmen Bell, BSP; Janice Burgess, BSP; Terry Damm, BSP; Karen Jensen, BSP, MSc; Jeff Taylor, BSP, PhD
December, 2012
Last Updated: February 2019